Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1.
暂无分享,去创建一个
J. D. Clark | M. Hegen | Betsy S. Pierce | A. Gopalsamy | M. Dowty | F. Vajdos | J. Jussif | Fabien Vincent | L. Xing | Zhao‐Kui Wan | M. Banker | David C. Limburg | I. Efremov | E. Arnold | Xiaojing Yang | Andrew C Flick | Tsung H. Lin | Raman K. Sharma | C. Ambler | J. I. Trujillo | Xin Yang | Brian S. Gerstenberger | A. Fensome | R. Gifford | F. Vincent | J. Trujillo | J. Clark | T. Lin
[1] S. Spergel,et al. Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. , 2019, Journal of medicinal chemistry.
[2] W. Leonard,et al. The γc Family of Cytokines: Basic Biology to Therapeutic Ramifications. , 2019, Immunity.
[3] O. Silvennoinen,et al. Selective JAKinibs: Prospects in Inflammatory and Autoimmune Diseases , 2019, BioDrugs.
[4] D. S. Weinstein,et al. Advances in the Discovery and Development of Selective Tyrosine Kinase 2 (TK2) Inhibitors , 2018, 2018 Medicinal Chemistry Reviews.
[5] L. Olson,et al. In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494) , 2018, BMC Rheumatology.
[6] Li Xing,et al. Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841). , 2018, Journal of medicinal chemistry.
[7] K. Page,et al. The Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a TYK2/JAK1 Inhibitor (PF‐06700841) in Healthy Subjects and Patients With Plaque Psoriasis , 2018, Journal of clinical pharmacology.
[8] Alan Menter,et al. Anti‐IL‐23 and Anti‐IL‐17 Biologic Agents for the Treatment of Immune‐Mediated Inflammatory Conditions , 2018, Clinical pharmacology and therapeutics.
[9] Adam R. Johnson,et al. Resolving TYK2 locus genotype-to-phenotype differences in autoimmunity , 2016, Science Translational Medicine.
[10] M. Varma,et al. Predicting Clearance Mechanism in Drug Discovery: Extended Clearance Classification System (ECCS) , 2015, Pharmaceutical Research.
[11] J. Telliez,et al. ATP-mediated kinome selectivity: the missing link in understanding the contribution of individual JAK Kinase isoforms to cellular signaling. , 2014, ACS chemical biology.
[12] Mark E Flanagan,et al. Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases. , 2014, Journal of medicinal chemistry.
[13] M. Dowty,et al. Preclinical to Clinical Translation of Tofacitinib, a Janus Kinase Inhibitor, in Rheumatoid Arthritis , 2014, The Journal of Pharmacology and Experimental Therapeutics.
[14] Li Di,et al. Development of a new permeability assay using low-efflux MDCKII cells. , 2011, Journal of pharmaceutical sciences.
[15] R. Obach. Predicting clearance in humans from in vitro data. , 2011, Current topics in medicinal chemistry.
[16] J. Fridman,et al. Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050 , 2010, The Journal of Immunology.
[17] H. Kantarjian,et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. , 2010, Blood.
[18] D. N. Bobrov,et al. Stereochemistry of the Kulinkovich cyclopropanation of nitriles. , 2009, The Journal of organic chemistry.
[19] Bill J Smith,et al. Prediction of Human Pharmacokinetics From Preclinical Information: Comparative Accuracy of Quantitative Prediction Approaches , 2009, Journal of clinical pharmacology.
[20] M. Hegen,et al. Utility of animal models for identification of potential therapeutics for rheumatoid arthritis , 2007, Annals of the rheumatic diseases.
[21] Clifford Liongue,et al. Cytokine receptor signaling through the Jak-Stat-Socs pathway in disease. , 2007, Molecular immunology.